Syntheses and biological evaluation of indole-2 and 3-carboxamides: new selective cyclooxygenase-2 inhibitors

Pharmazie. 2002 Apr;57(4):238-42.

Abstract

A series of indol-2 and 3-carboxamides were prepared and evaluated for their ability to inhibit cyclooxygenase-2 (COX-2) and cyclooxygenase-1 (COX-1). Substitution on indol nitrogen with benzyl and p-fluorobenzyl group of indole-2 carboxamides 8, 10, 11 provides fairly active COX-2 enzyme inhibitors.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amides / chemical synthesis*
  • Amides / chemistry
  • Amides / pharmacology*
  • Chemical Phenomena
  • Chemistry, Physical
  • Cyclooxygenase 1
  • Cyclooxygenase 2
  • Cyclooxygenase 2 Inhibitors
  • Cyclooxygenase Inhibitors / chemical synthesis*
  • Cyclooxygenase Inhibitors / chemistry
  • Cyclooxygenase Inhibitors / pharmacology*
  • Drug Design
  • Humans
  • In Vitro Techniques
  • Indicators and Reagents
  • Indoles / chemical synthesis*
  • Indoles / chemistry
  • Indoles / pharmacology*
  • Isoenzymes / drug effects
  • Magnetic Resonance Spectroscopy
  • Membrane Proteins
  • Prostaglandin-Endoperoxide Synthases / drug effects

Substances

  • Amides
  • Cyclooxygenase 2 Inhibitors
  • Cyclooxygenase Inhibitors
  • Indicators and Reagents
  • Indoles
  • Isoenzymes
  • Membrane Proteins
  • Cyclooxygenase 1
  • Cyclooxygenase 2
  • PTGS1 protein, human
  • PTGS2 protein, human
  • Prostaglandin-Endoperoxide Synthases